2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1 ]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability
- Author
- VERHEIJEN, Jeroen C1 ; RICHARD, David J1 ; CURRAN, Kevin1 ; KAPLAN, Joshua1 ; YU, Ker2 ; ZASK, Arie1
[1] Chemical Sciences, Wyeth Research, 401 N. Middletown Rd, Pearl River, NY 10965, United States
[2] Oncology Research, Wyeth Research, 401 N. Middletown Rd, Pearl River, NY 10965, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2010, Vol 20, Num 8, pp 2648-2653, 6 p
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- Cancer Kinase inhibitors Microsomes Oncology P13K mTOR
- Keyword (fr)
- Animal Anticancéreux Carboxamide Cellule tumorale Chimiothérapie Composé bicyclique Cycle 6 chaînons Cytotoxicité Dérivé de la pipéridine Dérivé du benzène Dérivé du pyrane Epithélium Glande mammaire Glioblastome Homme Hétérocycle azote Hétérocycle oxygène azote Inhibiteur enzyme Lignée cellulaire Non-specific serine/threonine protein kinase Prostate Protéine mTOR Relation structure activité Souris Synthèse chimique Sélectivité Transduction signal Urées Voie intraveineuse 1,3,5-Triazine dérivé 8-Azabicyclo[3.2.1]octane dérivé Benzoïque acide4-[3-(4-[4-(3-oxa-8-azabicyclo[3.2.1 ]oct-8-yl)-6-(perhydropyran-4-yl)-1,3,5-triazin-2-yl]phényl)uréido] 4-isopropylpipéridide Lignée LNCAP Lignée MDAMB361 Lignée U87MG Stabilité métabolique Cancer Enzyme Gliome malin Mammalia Rodentia Traitement Transferases Tumeur maligne Vertebrata
- Keyword (en)
- Animal Antineoplastic agent Carboxamide Tumor cell Chemotherapy Bicyclic compound Six membered ring Cytotoxicity Piperidine derivatives Benzene derivatives Pyran derivatives Epithelium Mammary gland Glioblastoma Human Nitrogen heterocycle Oxygen nitrogen heterocycle Enzyme inhibitor Cell line Non-specific serine/threonine protein kinase Prostate Mammalian target of rapamycin Structure activity relation Mouse Chemical synthesis Selectivity Signal transduction Ureas Intravenous administration Metabolic stability Cancer Enzyme Malignant glioma Mammalia Rodentia Treatment Transferases Malignant tumor Vertebrata
- Keyword (es)
- Animal Anticanceroso Carboxamida Célula tumoral Quimioterapia Compuesto bicíclico Ciclo 6 eslabones Citotoxicidad Piperidina derivado Benceno derivado Pirano derivado Epitelio Glándula mamaria Glioblastoma Hombre Heterociclo nitrógeno Heterociclo oxígeno nitrógeno Inhibidor enzima Línea celular Non-specific serine/threonine protein kinase Prostata Proteína mTOR Relación estructura actividad Ratón Síntesis química Selectividad Transducción señal Ureas Vía intravenosa Cáncer Enzima Glioma maligno Mammalia Rodentia Tratamiento Transferases Tumor maligno Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02R Antineoplastic agents / 002B02R01 General aspects
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 22824979
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmcl.2010.02.031 
https://dx.doi.org/10.1016/j.bmcl.2010.02.031
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